FABRICATION OF TOPICAL BACLOFEN LOADED EMULGEL: CHARACTERIZATION, OPTIMIZATION USING 23 FULL FACTORIAL DESIGN AND IN VIVO ANTI-INFLAMMATORY ACTIVITY

Document Type : Original Article

Authors

1 Department of Pharmaceutics, Faculty of Pharmacy, October 6 University, 6th of October City, Egypt

2 Department of Pharmaceutics, Faculty of Pharmacy, Cairo University, Cairo, Egypt

3 Department of Pharmaceutics, Faculty of Pharmacy, October 6 University, 6th of October City, Egypt/ Department of Pharmaceutics, Faculty of Pharmacy, Cairo University, Cairo, Egypt

Abstract

Baclofen is a GABA-B receptors agonist and possesses anti-inflammatory properties. It has many gastrointestinal side effects and narrow therapeutic index. Thus, the objective of this study was to produce emulgel for the topical delivery of baclofen so as to evade its side effects. Emulgel containing 1% baclofen were fabricated, evaluated and optimized applying full factorial design (23). Liquid paraffin concentration, cremophor RH 40 concentration, and penetration enhancers type was selected as independent variables in the current study to determine the influence of them on the percentage release of baclofen after 30 minutes. The anti-inflammatory activity of the optimal baclofen emulgel was assessed employing the carragenan-induced rat paw edema method. The formulation E5 was established to fulfill the maximum requisite of an optimum formulation with desirability value of 0.982. The mean percentage inhibition value of E5 after 1 hour of application was significantly higher than Baclofen® tablet, baclofen hydrogel and Voltaren® emulgel. The % relative bioavailability of E5 was 108.9%, 99.8% and 138.6% relative to Baclofen® tablet, Voltaren® emulgel and baclofen hydrogel respectively. Therefore, baclofen emulgel can be utilized as an effective anti-inflammatory for topical drug delivery.

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